[Phe13,Tyr19]-MCH (human, mouse, rat) CAS NO. 160201-86-5

[Phe13,Tyr19]-MCH (human, mouse, rat) CAS NO. 160201-86-5

[Phe13,Tyr19]-MCH (human, mouse, rat)  CAS NO. 160201-86-5

[Phe13,Tyr19]-MCH (human, mouse, rat) CAS NO. 160201-86-5

[Phe13,Tyr19]-MCH (human, mouse, rat) CAS NO. 160201-86-5

[Phe13,Tyr19]-MCH is a synthetic, site-specifically modified analog of Melanin Concentrating Hormone (MCH), featuring phenylalanine at position 13 and tyrosine at position 19, within the conserved 19-amino acid cyclic structure (with a disulfide bridge) common to human, mouse, and rat MCH. These modifications are designed to enhance receptor binding affinity, proteolytic stability, or introduce spectroscopic probes (via the tyrosine residue) without fundamentally altering the peptide's core agonist activity. 



TECHNICAL SPECIFICATIONS


Item
Specification
Product Name
Biotin-Glucagon (1-29), bovine, human, porcine
CAS NO.
/
Appearance
White to off-white lyophilized powder
Molecular Formula
C163H239N45O51S2
Molecular Weight
3709.12g/mol 
Purity (RP-HPLC)
≥ 95.0%
Solubility

Soluble in water (≥ 5 mg/mL), dilute acetic acid, or DMSO; also soluble in phosphate-buffered saline (PBS)

Endotoxin≤1.0 EU/mg
Biological Activity
 Binds to glucagon receptors with high affinity; EC₅₀ typically ≤ 0.5 nM in cAMP accumulation assays using hepatocyte or CHO cell models
Storage Conditions
Store at -20°C to -80°C in a dry, dark environment; avoid repeated freeze-thaw cycles.
Stock Location
Stock in USA
MOQ
1g


1.MECHANISM OF ACTION

This analog functions as a potent agonist for the Melanin Concentrating Hormone Receptor 1 (MCHR1). The modifications at positions 13 and 19 are strategically chosen to optimize interactions with the receptor binding pocket. The aromatic side chain of phenylalanine at position 13 may enhance hydrophobic interactions, while tyrosine at position 19 can improve receptor engagement or serve as a site for iodination or other labeling. Like native MCH, it binds to MCHR1, a G protein-coupled receptor, and primarily activates Gi/o signaling. 


    2.PRODUCT INDICATIONS

  • Enhanced Receptor Binding Studies: Used in competitive binding assays to study MCHR1 due to potentially higher affinity or altered binding kinetics compared to the native peptide.

  • Structure-Activity Relationship (SAR) Research: Investigating the contribution of specific amino acid residues (positions 13 and 19) to receptor interaction, activation, and stability.

  • Peptide Stability & Metabolism Studies: Assessing if the modifications confer increased resistance to enzymatic degradation, leading to a longer duration of action in in vivoor ex vivoexperiments.

  • Radioligand Development: The tyrosine residue at position 19 provides a convenient site for radioiodination (e.g., with I-125), enabling the creation of a high-specific-activity radioligand for detailed receptor autoradiography, binding saturation, and competition experiments.


    3.CLINICAL EFFICACY OF PRODUCT

  • Research & Tool Efficacy: Its "efficacy" is defined by its performance in the laboratory as a potentially superior reagent—offering higher affinity, greater stability, or unique labeling capabilities—for dissecting the MCH/MCHR1 system compared to the native peptide.

  • Drug Design Insights: Research on such analogs provides crucial information on the pharmacophore of MCH—the specific chemical features required for receptor binding and activation. This knowledge directly informs the rational design of non-peptide, drug-like MCHR1 antagonists or agonists.

  • Therapeutic Target Context: The MCH system, validated by analogs like this one, remains a target for drug discovery in obesity and mood disorders. Understanding how modifications affect peptide function helps medicinal chemists design stable, bioavailable small molecules.

  • Clinical Status: No modified MCH peptide analogs are in clinical use. The clinical pipeline has focused on oral small-molecule MCHR1 antagonists, none of which have been approved to date. This analog's value is entirely confined to preclinical research and drug development stages.


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